Tolvaptan (kidney disease)
Tolvaptan (Jynarque) is a prescription tablet used to slow the loss of kidney function in adults with rapidly progressing autosomal dominant polycystic kidney disease (ADPKD).
🧬 Where this information comes from Click to expand
The clinical label records used on this page are FDA-filed Structured Product Labeling (SPL) retrieved through openFDA. We identified 1 clinical label set within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. Forms, routes, brands, labelers, strengths, and NDC product-record counts are built separately from matching FDA National Drug Code Directory records. The linked DailyMed document is a representative official source for verification, not the page’s only clinical source. View the linked label on DailyMed →
Tolvaptan (Jynarque) is a specialist medicine that can meaningfully slow kidney function loss in adults with rapidly progressing autosomal dominant polycystic kidney disease (ADPKD), by blocking vasopressin, the hormone that tells kidneys to hold on to water and also drives cyst growth. Expect intense thirst and frequent urination, night included; that is the drug working, not a fault, and it is often the hardest part, so keep water with you all day. It carries a boxed warning for serious, potentially fatal liver injury, so liver blood tests continue for as long as you take it, and yellowing skin or eyes or dark urine means stop and call your prescriber.
Clinical pearls
- Jynarque is dispensed only through a restricted safety program (REMS), so it usually comes from an enrolled specialty pharmacy.
- Avoid grapefruit juice, and flag tolvaptan whenever you are prescribed antifungals or antibiotics, since some sharply raise its levels.
- Take the larger dose on waking and the smaller one about 8 hours later, so nighttime urination stays manageable.
- Tolvaptan cancels out desmopressin (used for bedwetting or diabetes insipidus), so the two should not be used together.
⚠️ FDA Boxed Warning — the FDA’s strongest safety alert ▾
Tolvaptan (Jynarque) can cause serious, potentially life-threatening liver damage — including liver failure that has required a liver transplant. This is not a minor side effect; it is a real risk that must be taken seriously. Before you start this medication, your doctor will check your liver with blood tests (ALT, AST, and bilirubin). Those tests must continue at 2 weeks, 4 weeks, then every month for 18 months, and then every 3 months after that — for as long as you take the drug.
Watch for warning signs of liver trouble: fatigue, loss of appetite, nausea, vomiting, fever, rash, itching, yellowing of the skin or eyes, or dark-colored urine. Report any of these to your doctor immediately. Because of this liver risk, tolvaptan is only dispensed through a special safety program (REMS) — not every pharmacy can fill it.
Patient information guide A plain-language walkthrough of Tolvaptan (kidney disease), written from its FDA label.
What Tolvaptan (kidney disease) is used for
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Tolvaptan (Jynarque) is used to slow the loss of kidney function in adults with ADPKD who are at risk of rapid disease progression.
- Autosomal dominant polycystic kidney disease (ADPKD) — slows the rate at which kidney function declines in adults whose kidneys are deteriorating quickly
How Tolvaptan (kidney disease) works
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Your kidneys have receptors that respond to a hormone called vasopressin (also known as ADH — antidiuretic hormone). In ADPKD, vasopressin signals drive cyst growth and fluid buildup in the kidney. Tolvaptan blocks the vasopressin V2 receptor, cutting off this signal. This lowers a chemical inside kidney cells called cAMP, which in turn slows cyst growth and fluid secretion into cysts — and causes the kidneys to release more water in the urine (aquaresis).
In lab studies using human ADPKD cyst cells, tolvaptan directly inhibited cyst growth. In animal models, reduced cAMP levels were linked to slower growth of total kidney volume and fewer new cysts forming.
Tolvaptan (kidney disease) dosage
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Tolvaptan is taken orally (by mouth) as a tablet, twice a day — a larger dose in the morning on waking and a smaller dose 8 hours later. It can be taken with or without food, though a very high-fat meal may raise peak levels. Your doctor will start you at a lower total daily dose and increase it over time as your body tolerates it, with at least a week between dose increases.
- Take the morning dose when you wake up; take the second dose 8 hours later
- If you miss a dose, skip it — take the next dose at its scheduled time; never double up
- Drink plenty of fluids throughout the day to avoid thirst and dehydration
- Avoid grapefruit juice while taking this medication
Dosing details from the FDA-approved label
From the Tolvaptan (kidney disease) prescribing information (“Dosage and Administration”). Doses are set by your prescriber for your product, condition, kidney function and age — never change a dose on your own.
Titrate to 60 mg plus 30 mg then to 90 mg plus 30 mg per day if tolerated with at least weekly intervals between titrations.
Read the label’s full dosing text
2 DOSAGE AND ADMINISTRATION Recommended dosage ( 2.1 ) Initial Dosage Titration Step Target Dosage 1st Dose 45 mg 1st Dose 60 mg 1st Dose 90 mg 2nd Dose (8 hours later) 15 mg 2nd Dose (8 hours later) 30 mg 2nd Dose (8 hours later) 30 mg Total Daily Dose 60 mg Total Daily Dose 90 mg Total Daily Dose 120 mg Dose adjustment is recommended for patients taking moderate CYP3A inhibitors ( 2.4 , 5.4 , 7.1 ) 2.1 Recommended Dosage The initial dosage for JYNARQUE is 60 mg orally per day as 45 mg taken on waking and 15 mg taken 8 hours later. Titrate to 60 mg plus 30 mg then to 90 mg plus 30 mg per day if tolerated with at least weekly intervals between titrations. Patients may down-titrate based on tolerability. Encourage patients to drink enough water to avoid thirst or dehydration. 2.2 Monitoring To mitigate the risk of significant or irreversible liver injury, perform blood testing for ALT, AST and bilirubin prior to initiation of JYNARQUE, at 2 and 4 weeks after initiation, monthly for 18 months and every 3 months thereafter . Monitor for concurrent symptoms that may indicate liver injury [see Warnings and Precautions (5.1) ] . 2.3 Missed Doses If a dose of JYNARQUE is not taken at the scheduled time, take the next dose at its scheduled time. 2.4 Co-Administration with CYP3A Inhibitors CYP3A Inhibitors Concomitant use of strong CYP3A inhibitors is contraindicated [see Contraindications (4) and Warnings and Precautions (5.4) ] . In patients taking concomitant moderate CYP3A inhibitors, reduce the dose of JYNARQUE per Table 1. Consider further reductions if patients cannot tolerate the reduced dose [see Warnings and Precautions (5.4) and Drug Interactions (7.1) ] . Interrupt JYNARQUE temporarily for short term therapy with moderate CYP3A inhibitors if the recommended reduced doses are not available. Table 1: Dose adjustment for patients taking moderate CYP3A inhibitors Standard Morning and Afternoon Dose (mg) Dose (mg) with Moderate CYP3A Inhibitors 90 mg and 30 mg 45 mg and 15 mg 60 mg and 30 mg 30 mg and 15 mg 45 mg and 15 mg 15 mg and 15 mg
Read the full Dosage and Administration section on DailyMed →
Tolvaptan (kidney disease) side effects
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The most common side effects with tolvaptan — reported in more than 10% of patients — are all related to its strong water-releasing effect:
Common side effects
- Increased thirst
- Frequent urination (polyuria)
- Urinating during the night (nocturia)
- Needing to urinate more often (pollakiuria)
- Excessive fluid intake to compensate (polydipsia)
- Fatigue
- Nausea
- Decreased appetite
When to get medical help
- Signs of liver damage: fatigue, nausea, loss of appetite, pain in the upper right abdomen, vomiting, fever, rash, itching, yellowing of the skin or eyes (jaundice), or dark urine — stop the medication and contact your doctor immediately
- Signs of high sodium in the blood (hypernatremia): extreme thirst, confusion, weakness — seek medical attention
- Signs of dehydration or low blood volume: dizziness, light-headedness, or feeling faint — contact your doctor
Serious reactions — including liver injury (see warning below) and dehydration — require prompt medical attention. Stop the medication and call your doctor right away if you develop jaundice (yellowing of skin or eyes), dark urine, right-sided belly pain, or feel extremely dizzy or faint.
Tolvaptan (kidney disease) warnings and precautions
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- Serious liver injury: Tolvaptan can cause liver failure, including cases requiring transplantation. Regular liver blood tests are required before starting and throughout treatment. Stop the drug and call your doctor immediately if you notice yellowing of the skin or eyes, dark urine, upper right abdominal pain, fatigue, nausea, vomiting, fever, rash, or itching.
- High blood sodium (hypernatremia) and dehydration: Because tolvaptan causes heavy urination, blood sodium can rise and you can become dehydrated. Drinking enough water every day is essential. This drug is not safe for people who cannot feel or respond to thirst, or who are already dehydrated.
- Restricted availability (REMS program): Tolvaptan is only available through a special safety program. Your prescriber and pharmacy must both be enrolled. You will also need to be enrolled as a patient.
- Drug interactions: Strong CYP3A-inhibiting medications must not be taken with tolvaptan — they can dramatically raise drug levels in your body to dangerous amounts.
Tolvaptan (kidney disease) interactions
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Tolvaptan is broken down by an enzyme in the liver called CYP3A. Drugs that affect this enzyme can significantly change how much tolvaptan stays in your body:
- Strong CYP3A inhibitors (e.g., certain antifungals, some antibiotics): Contraindicated — cannot be used together; they can raise tolvaptan levels to dangerous amounts
- Moderate CYP3A inhibitors: Require a dose reduction of tolvaptan; your doctor will adjust your dose
- Strong CYP3A inducers (e.g., rifampin, certain anti-seizure drugs): Reduce tolvaptan levels, making it less effective — avoid combining
- Desmopressin (dDAVP): Tolvaptan blocks the same receptor that desmopressin activates, making desmopressin ineffective — avoid combining
- Grapefruit juice: Can increase tolvaptan blood levels — avoid while on this medication
Interactions listed in the FDA-approved label
From the Tolvaptan (kidney disease) prescribing information (“Drug Interactions”): what the manufacturer studied or reported to the FDA.
Avoid concomitant use with: Strong CYP3A Inducers ( 7.1 ) V 2 -Receptor Agonists ( 7.2 ) 7.1 CYP3A Inhibitors and Inducers CYP3A Inhibitors Tolvaptan's AUC was 5.4 times as large and Cmax was 3.5 times as large after co-administration of tolvaptan and 200 mg ketoconazole [see Warnings and Precautions (5.4) and Clinical Pharmacology (12.3) ] . Larger doses of the strong CYP3A inhibitor would be expected to produce…
Read the label’s full interactions text
7 DRUG INTERACTIONS Avoid concomitant use with: Strong CYP3A Inducers ( 7.1 ) V 2 -Receptor Agonists ( 7.2 ) 7.1 CYP3A Inhibitors and Inducers CYP3A Inhibitors Tolvaptan's AUC was 5.4 times as large and Cmax was 3.5 times as large after co-administration of tolvaptan and 200 mg ketoconazole [see Warnings and Precautions (5.4) and Clinical Pharmacology (12.3) ] . Larger doses of the strong CYP3A inhibitor would be expected to produce larger increases in tolvaptan exposure. Concomitant use of tolvaptan with strong CYP3A inhibitors is contraindicated [see Contraindications (4) ]. Dose reduction of JYNARQUE is recommended for patients while taking moderate CYP3A inhibitors [see Dosage and Administration (2.4) ]. Patients should avoid grapefruit juice beverages while taking JYNARQUE. Strong CYP3A Inducers Co-administration of JYNARQUE with strong CYP3A inducers reduces exposure to JYNARQUE [see Clinical Pharmacology (12.3) ]. Avoid concomitant use of JYNARQUE with strong CYP3A inducers [see Dosage and Administration (2.4) ]. 7.2 V 2 -Receptor Agonist As a V 2 -receptor antagonist, tolvaptan will interfere with the V 2 -agonist activity of desmopressin (dDAVP). Avoid concomitant use of JYNARQUE with a V 2 -agonist.
Not a complete list. The label covers the interactions the manufacturer studied or reported, and our own interaction database does not cover every medicine either. Bring your full medication list, including vitamins and herbal products, to your pharmacist.
Before taking Tolvaptan (kidney disease)
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- Do not take tolvaptan if you have a history of significant liver disease or liver injury (does not apply to uncomplicated polycystic liver disease)
- Do not take it if you are currently on a strong CYP3A inhibitor
- Do not take it if your blood sodium levels are abnormally high or low and uncorrected
- Do not take it if you cannot feel thirst or respond to it
- Do not take it if you have urinary blockage or produce no urine (anuria)
- Do not take it if you are already significantly dehydrated (hypovolemic)
- Pregnancy: May harm the fetus — tell your doctor if you are pregnant or planning to become pregnant
- Breastfeeding: Not recommended while taking this medication
- Tell your doctor about all medications, supplements, and herbal products you take — especially anything affecting the liver or kidneys
Tolvaptan (kidney disease) overdose
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If too much tolvaptan is taken, the expected effects would be an exaggerated version of what the drug normally does: a large rise in blood sodium, heavy urination, intense thirst, and dehydration or low blood volume. There is no specific antidote. If an overdose is suspected, monitoring of vital signs, blood electrolytes, heart rhythm (ECG), and fluid status is recommended, and fluids and electrolytes should be replaced until the excess urination subsides.
Dialysis is unlikely to be helpful because tolvaptan binds very tightly to proteins in the blood (more than 98%), making it difficult to remove through that method.
What Tolvaptan (kidney disease) does in the body
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Tolvaptan starts increasing urine output within 1 to 2 hours of a dose. The effect peaks between 4 and 8 hours after taking it, then gradually returns to baseline within 24 hours. With the recommended twice-daily dosing, the vasopressin receptor in the kidney stays blocked for the entire day — shown by sustained increased urine output and lower urine concentration (osmolality) throughout the day.
Because so much extra water is lost in the urine, blood sodium levels can rise unless you drink enough fluids to replace what's lost. In patients with higher baseline kidney function, the urinary effects are more pronounced.
How your body processes Tolvaptan (kidney disease)
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After an oral dose, tolvaptan reaches peak blood levels within 2 to 4 hours. It can be taken with or without food, though a high-fat meal roughly doubles the peak concentration (while the total amount absorbed stays the same). Tolvaptan binds very tightly to proteins in the blood (more than 98%). It is metabolized mainly in the liver by an enzyme called CYP3A, and its breakdown products have little to no activity at the vasopressin receptor.
How to store Tolvaptan (kidney disease)
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Store at 20°C to 25°C (68°F to 77°F), excursions permitted between 15°C and 30°C (59°F to 86°F) .
Written from the FDA-approved label with AI and reviewed by our pharmacy team. How we use AI →
Supplements & herbs that interact with Tolvaptan (kidney disease)
145 supplements and herbal products have documented interactions with Tolvaptan (kidney disease) in the licensed clinical database we use. Most are manageable — but your pharmacist should know about everything you take, including vitamins and herbals.
- Major · 3
- Moderate · 104
- Minor · 38
Educational information from a licensed clinical database (Natural Medicines) — see our data sources & update cadence. Not medical advice: an interaction being documented does not mean it will happen to you; do not start or stop medications or supplements without professional guidance.
Tolvaptan (kidney disease): pharmacist answers to common questions
Quick, plain-English answers to the questions patients ask most about Tolvaptan (kidney disease) — the kind of thing our pharmacy team would talk through with you at the counter.
What exactly is this medication doing for my kidneys?
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I've heard this drug can hurt my liver. How serious is that?
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Why am I going to the bathroom so much more? Is that normal?
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Are there any medications or foods I need to avoid while on this?
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Is it safe to take tolvaptan if I'm pregnant or thinking about getting pregnant?
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Why do I have to get this prescription through a special program? I can't just pick it up anywhere?
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Is Tolvaptan (kidney disease) available over the counter?
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When was Tolvaptan (kidney disease) first available?
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Answers drafted from the FDA-approved label with AI and reviewed by our pharmacy team. How we use AI →
More about Tolvaptan (kidney disease) on HelloPharmacist
Tolvaptan (kidney disease) on the U.S. market: products, makers and brands
How Tolvaptan (kidney disease) appears in the FDA’s National Drug Code Directory — including its dosage forms, strengths, brand names, manufacturers, and FDA-listed product records. These are directory records, not sales or prescription volume.
The FDA lists Tolvaptan (kidney disease) products; the earliest marketing or approval year on record is 2009. Brand names on the directory include Jynarque, Samsca; the rest are generics.
How widely Tolvaptan (kidney disease) is used (Medicaid data)
A general measure of how commonly Tolvaptan (kidney disease) is prescribed, based on Medicaid — one of the largest public drug programs. The figure below is prescriptions filled in Q1–Q4 2025, summed across every form and brand of the drug.
Think of this as a proxy for how widely Tolvaptan (kidney disease) is used, drawn from freely available public data. Medicaid is just one program — these numbers don’t include Medicare, other government coverage, or commercial and cash-pay prescriptions, so real-world use is higher than what’s shown here.
How commonly is Tolvaptan (kidney disease) prescribed? Of the 1,601 medications we measure, Tolvaptan (kidney disease) ranks #1,028 by Medicaid prescriptions — more than 36% of them.
Utilization by Tolvaptan (kidney disease) product
Pick a product to see its own Medicaid numbers. Each chip is one clinical product — a specific strength & dosage form as defined by RxNorm — with brand-name and generic versions combined.
Hyponatremia tolvaptan 15 MG Oral Tablet Most dispensed
Summed across the 3 of 17 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 849827
Hyponatremia tolvaptan 30 MG Oral Tablet
Summed across the 1 of 17 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 849833
Other Tolvaptan (kidney disease) products — combination packs and listings not yet matched to a specific clinical product (kept visible so every prescription is accounted for)
Summed across the 9 of 20 listed NDC products with Medicaid activity.
Shares are of the Medicaid prescriptions shown here. Product grouping follows RxNorm (the National Library of Medicine’s drug terminology), so “one product” means one strength & dosage form regardless of manufacturer. Dollar figures are gross Medicaid reimbursement before mandatory rebates — rebates (often large, especially for brand-name drugs) are confidential, so actual net cost to Medicaid is lower than shown.
Source: Medicaid State Drug Utilization Data (CMS), aggregated by generic ingredient — summed across every NDC (all brands, strengths, salt forms and dosage forms) of Tolvaptan (kidney disease), and across all states and both fee-for-service and managed-care claims. A general popularity signal; it excludes Medicare, commercial insurance and cash prescriptions, so it is not total U.S. use. Based on the 13 of 54 listed Tolvaptan (kidney disease) NDCs with Medicaid activity.
Tolvaptan (kidney disease) side effects reported to the FDA (FAERS)
After a medicine reaches the market, patients, doctors and drugmakers can send the FDA reports of problems they think may be linked to it. Here’s what’s been reported for Tolvaptan (kidney disease) — a signal of what to watch for, not proof the drug caused it.
Source: openFDA, from the FDA Adverse Event Reporting System (FAERS). These are voluntary reports — they don’t prove the drug caused the effect, and counts reflect how often something was reported, not how often it actually happens. Reports also often name the very problem the medicine is taken for — a common reason to file one is that the drug didn’t help — so for a pain reliever you may see “pain” high on the list; that points to why the report was filed, not to the drug causing the symptom. This counts every report that lists Tolvaptan (kidney disease) in any role, so the total runs higher than the FDA’s official dashboard, which counts only cases where the drug is the suspect. For the authoritative figures, see the FDA FAERS Public Dashboard. Always talk to your pharmacist or doctor.
Tolvaptan (kidney disease) FDA approval history
How Tolvaptan (kidney disease) went from FDA review to the pharmacy shelf — the key milestones in its regulatory journey.
Source: Drugs@FDA.
Tolvaptan (kidney disease) recall history
A recall is when a specific batch of a medicine is pulled from the market — usually a manufacturing issue, not a problem with the drug itself. Class I is most serious, Class III least.
The FDA’s enforcement reports list no Tolvaptan recalls since July 2021.
✅No Tolvaptan recalls on record since July 2021Source: FDA enforcement (recall) reports, via openFDA; our copy was last updated Sep 24, 2026.
RxNorm Concept Web — From Ingredient to Every Form and Strength
This page starts with one ingredient concept (IN). The branches below show its dose-form concepts (SCDF), then the available clinical drug and strength concepts (SCD). Combination products remain separate concepts with their own pages.
RxCUI 358257 1 dose form · 7 strengths
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Dose form (SCDF) Oral Tablet RxCUI 849826No current FDA listingClinical drug / strength (SCD) Hyponatremia tolvaptan 15 MGRxCUI 849827Hyponatremia tolvaptan 30 MGRxCUI 84983315 MGRxCUI 271933530 MGRxCUI 271933745 MGRxCUI 204435960 MGRxCUI 204436390 MGRxCUI 2044367
Look up RxCUI 358257 in the RxCUI Atlas →
RxNorm is the U.S. National Library of Medicine’s normalized drug vocabulary. Its concept hierarchy can include forms that are not currently marketed; the status on each branch compares that concept with current FDA listings. RxCUIs identify vocabulary concepts, not individual packages or manufacturers.
Tolvaptan (kidney disease) supply and shortage status
Whether Tolvaptan (kidney disease) is in short supply in the U.S. right now, plus any shortage history the FDA has on record. A shortage usually reflects a manufacturing or demand issue — not a safety problem with the drug.
Source: openFDA, from the FDA Drug Shortages database.
Tolvaptan (kidney disease) brand names
Tolvaptan (kidney disease) is sold under 2 brand names in the FDA directory — Jynarque, Samsca. A brand and its generic contain the same active ingredient; the brand name belongs to one company's product.
Tolvaptan (kidney disease) drug class (RxNorm)
Tolvaptan (kidney disease) belongs to the Vasopressin V2 Receptor Antagonist class.
Classified by RxNorm RxClass — the U.S. National Library of Medicine's standardized drug-classification service (Established Pharmacologic Class from the FDA, the ATC drug family from the WHO, and mechanism of action). Reference only, not medical advice.
Sources for this Tolvaptan (kidney disease) page
Core label, product, RxNorm, safety, and utilization data on this page come from the sources identified below. AI-written, editorial, and licensed sections are labeled separately.
How this page is built
HelloPharmacist combines public FDA and NLM records and does not author the underlying clinical facts. The plain-language sections are written with AI from the FDA-approved label text and reviewed by our pharmacy team before publication. Otsuka America Pharmaceutical, Inc. is the representative DailyMed label linked for verification and dates. This is general education, not medical advice: always talk to your doctor or pharmacist about your own medicines. How we build and review drug pages →